Patent classifications
C07D215/00
Trans-indoline cyclopropylamine chemical compound, and method for preparation, pharmaceutical composition, and use thereof
The present invention relates to the fields of medicinal chemistry and pharmacotherapy, and specifically relates to the chemical compound of formula (I), and its racemate, R-isomer, S-isomer, pharmaceutically acceptable salt, and mixtures thereof, as well as its method for preparation, a pharmaceutical composition containing said chemical compound, and use as a lysine-specific demethylase 1 (LSD 1) inhibitor. The cyclopropylamine chemical compound to which the present invention relates may be used in the treatment of cancer. ##STR00001##
Antibacterial compounds and uses thereof
The present invention relates to compounds of formula (I) including any stereochemically isomeric form thereof, or pharmaceutically acceptable salts thereof, for the treatment of tuberculosis. ##STR00001##
Crystalline solid forms of N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N′-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, processes for making, and methods of use
The invention relates to novel crystalline solid forms of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide (Compound 1), and solvates thereof, including hydrates, that are useful for the treatment of cancer. Also disclosed are pharmaceutical compositions comprising the crystalline solid forms and processes for making the crystalline solid forms, as well as methods of using them for the treatment of cancer, particularly thyroid cancer, prostate cancer, hepatocellular cancer, renal cancer, and non-small cell lung carcinoma. The crystalline solid forms can be used to make the L-malate salt of cabozantinib.
Core-shell structure supported tungsten composite catalyst and preparation method and use thereof
The present invention discloses a core-shell structure supported tungsten composite catalyst and a preparation method and use thereof. Most of the existing synthesis methods of the main ring of quinolone drugs have the defects of many synthesis steps, cumbersome operation, large amount of three wastes, higher costs and the like. The present invention prepares a magnetic separable core-shell supported tungsten composite catalyst, WO.sub.3/SiO.sub.2/Fe.sub.3O.sub.4, by preparing Fe.sub.3O.sub.4 colloid and SiO.sub.2/Fe.sub.3O.sub.4 composite nano-particles. This magnetic separable core-shell supported tungsten composite catalyst, WO.sub.3/SiO.sub.2/Fe.sub.3O.sub.4, is used to catalyze and synthesize quinolone compounds. The present invention provides an efficient preparation method of quinolone compounds using a catalyst which can be recovered by magnetic separation and recycled. The catalyst prepared by the present invention can be reused in the preparation of quinolone compounds and still retains the original activity without deactivation, which not only greatly improves the production efficiency, but also reduces the environmental pollution.
PRODRUGS OF NH-ACIDIC COMPOUNDS
The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.
PRODRUGS OF NH-ACIDIC COMPOUNDS
The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.
NEW COMPOUND HAVING FGFR INHIBITORY ACTIVITY AND PREPARATION AND APPLICATION THEREOF
A new compound having an FGFR inhibitory activity and preparation and application thereof are provided. In particular, the compound according to the invention has a structure as shown in formula I, in which each group and substituent are as defined in the description. Also, a preparation method for the compound and a use thereof in preparation of a drug for treating and/or preventing a tumor-related disease and/or an FGFR-related disease are provided.
##STR00001##
Protein tyrosine phosphatases or SHP2 inhibitors and uses thereof
Small molecule compounds derived from -sulfophenylacetic amide (SPAA) are provided as novel sulfonic acid based pTyr mimetics. These compounds effectively inhibit a variety of protein tyrosine phosphatases (PTPs), such as mPTPA, mPTPB, LMWPTP, and Laforin. Use of these compounds as pharmaceutical agents for treating diseases associated with abnormal protein tyrosine phosphatase activity is also provided.
SOLID STATE FORMS OF LENVATINIB MESYLATE
The present invention provides a crystalline form of Lenvatinib Mesylate, processes for the preparation of crystalline form of lenvatinib Mesylate and pharmaceutical compositions thereof. The crystalline form of lenvatinib Mesylate designated as Form VN1 is characterized by powder X-ray diffraction pattern. The present invention further provides a process for the preparation of amorphous form of lenvatinib Mesylate. The amorphous form is characterized by powder X-ray diffraction pattern.
Pharmaceutical compositions for the treatment of cystic fibrosis transmembrane conductance regulator mediated diseases
The present invention features compositions comprising a plurality of therapeutic agents wherein the presence of one therapeutic agent enhances the properties of at least one other therapeutic agent. In one embodiment, the therapeutic agents are cystic fibrosis transmembrane conductance regulators (CFTR) such as a CFTR corrector or CFTR potentiator for the treatment of CFTR mediated diseases such as cystic fibrosis. Methods and kits thereof are also disclosed.